Data from: Green approach for synthesis of bioactive Hantzsch 1,4-dihydropyridine derivatives based on thiophene moiety via multicomponent reaction

A novel green and efficient one-pot multicomponent synthesis of dihydropyridine derivatives in good to excellent yield were reported. In presence of CAN catalyst, different 1,3-dione and same starting material as 5-bromothiophene-2-carboxaldehyde and ammonium acetate were used under solvent and heat free (at room temperature) condition for the Hantzsch pyridine synthesis within short period of time. All compounds were evaluated for their in vitro antibacterial and antifungal activity and interestigly we found that 5b to 5f shows excellent activity than Ampicilin, whereas only 5e compound shows excellent antifungal activity against C.albicans compared to graseofulvin. The cyto-toxicity of all compounds has been assessed against Breast tumor cell lines (BT-549) but no activity was found. The X- ray structure of one such compound 5a viewing colourless block crystal was corresponded accurately to a primitive monoclinic cell.

本研究报道了一种绿色高效的一锅法多组分合成二氢吡啶衍生物的新方法，产物收率良好至优异。该反应以硝酸铈铵（Ceric Ammonium Nitrate, CAN）为催化剂，以不同的1,3-二酮、以及5-溴噻吩-2-甲醛和乙酸铵作为共用起始原料，在无溶剂、室温无加热条件下，通过汉奇吡啶合成反应可在短时间内完成。对所有化合物进行了体外抗菌及抗真菌活性评价，有趣的是，我们发现5b至5f的活性均优于氨苄西林（Ampicillin）；相较于灰黄霉素（Griseofulvin），仅化合物5e对白色念珠菌（Candida albicans, C. albicans）表现出优异的抗真菌活性。针对所有化合物的细胞毒性，我们以乳腺肿瘤细胞系（BT-549）为模型进行了评估，但未检测到活性。化合物5a的无色块状晶体的X射线衍射结构经解析后，与原始单斜晶胞的参数准确吻合。